Marine Drugs最新文献

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Ameliorative Effect of Chitosan/Spirulina platensis Ethanolic Extract Nanoformulation against Cyclophosphamide-Induced Ovarian Toxicity: Role of PPAR-γ/Nrf-2/HO-1 and NF-kB/TNF-α Signaling Pathways 壳聚糖/刺五加乙醇提取物纳米制剂对环磷酰胺诱导的卵巢毒性的改善作用:PPAR-γ/Nrf-2/HO-1 和 NF-kB/TNF-α 信号通路的作用
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-30 DOI: 10.3390/md22090395
May Almukainzi, Thanaa A. El-Masry, Hanaa A. Ibrahim, Hebatallah M. Saad, Enas I. El Zahaby, Asmaa Saleh, Maysa M. F. El-Nagar
{"title":"Ameliorative Effect of Chitosan/Spirulina platensis Ethanolic Extract Nanoformulation against Cyclophosphamide-Induced Ovarian Toxicity: Role of PPAR-γ/Nrf-2/HO-1 and NF-kB/TNF-α Signaling Pathways","authors":"May Almukainzi, Thanaa A. El-Masry, Hanaa A. Ibrahim, Hebatallah M. Saad, Enas I. El Zahaby, Asmaa Saleh, Maysa M. F. El-Nagar","doi":"10.3390/md22090395","DOIUrl":"https://doi.org/10.3390/md22090395","url":null,"abstract":"Cyclophosphamide (CP) is an anticancer drug that causes infertility disorders. This study was designed to evaluate a nanoformulation of chitosan with an ethanolic extract from Spirulina platensis in terms of its protection against cyclophosphamide-induced ovarian toxicity. Nine groups of female Wistar rats were randomly assigned as follows: 1: control vehicle, 2: chitosan polymer, 3: telmisartan, 4: Spirulina platensis extract, 5: nanoformulation of the Spirulina platensis, and 6: single injection of CP; groups 7, 8, and 9 received the same treatments as those used in groups 3, 4, and 5, respectively, with a single dose of CP (200 mg/kg, I.P). The results displayed that the CP treatment decreased estradiol, progesterone, anti-mullerian hormone, and GSH content, and it downregulated PPAR-γ, Nrf-2, and HO-1 gene expression. In addition, the CP treatment caused an increase in the FSH, LH, and MDA levels. In the same manner, the protein expression of caspase-3, NF-kB, and TNF-α was upregulated in response to the CP treatment, while PPAR-γ was downregulated in comparison with the control. The rats treated with SPNPs exhibited a substantial reduction in the detrimental effects of oxidative stress and inflammation of the ovarian tissue. This study’s conclusions showed that SPNPs counteracted the effects of CP, preventing the death of ovarian follicles and restoring the gonadotropin hormone balance and normal ovarian histological appearance.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211368","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Bioactive Glial-Derived Neurotrophic Factor from a Safe Injectable Collagen–Alginate Composite Gel Rescues Retinal Photoreceptors from Retinal Degeneration in Rabbits 安全注射型胶原-藻酸盐复合凝胶中的生物活性胶质细胞神经营养因子能拯救兔子视网膜光感受器,使其免于视网膜退化
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-30 DOI: 10.3390/md22090394
Tingyu Hu, Ting Zhou, Rajesh Kumar Goit, Ka Cheung Tam, Yau Kei Chan, Wai-Ching Lam, Amy Cheuk Yin Lo
{"title":"Bioactive Glial-Derived Neurotrophic Factor from a Safe Injectable Collagen–Alginate Composite Gel Rescues Retinal Photoreceptors from Retinal Degeneration in Rabbits","authors":"Tingyu Hu, Ting Zhou, Rajesh Kumar Goit, Ka Cheung Tam, Yau Kei Chan, Wai-Ching Lam, Amy Cheuk Yin Lo","doi":"10.3390/md22090394","DOIUrl":"https://doi.org/10.3390/md22090394","url":null,"abstract":"The management of vision-threatening retinal diseases remains challenging due to the lack of an effective drug delivery system. Encapsulated cell therapy (ECT) offers a promising approach for the continuous delivery of therapeutic agents without the need for immunosuppressants. In this context, an injectable and terminable collagen–alginate composite (CAC) ECT gel, designed with a Tet-on pro-caspase-8 system, was developed as a safe intraocular drug delivery platform for the sustained release of glial-cell-line-derived neurotrophic factor (GDNF) to treat retinal degenerative diseases. This study examined the potential clinical application of the CAC ECT gel, focusing on its safety, performance, and termination through doxycycline (Dox) administration in the eyes of healthy New Zealand White rabbits, as well as its therapeutic efficacy in rabbits with sodium-iodate (SI)-induced retinal degeneration. The findings indicated that the CAC ECT gel can be safely implanted without harming the retina or lens, displaying resistance to degradation, facilitating cell attachment, and secreting bioactive GDNF. Furthermore, the GDNF levels could be modulated by the number of implants. Moreover, Dox administration was effective in terminating gel function without causing retinal damage. Notably, rabbits with retinal degeneration treated with the gels exhibited significant functional recovery in both a-wave and b-wave amplitudes and showed remarkable efficacy in reducing photoreceptor apoptosis. Given its biocompatibility, mechanical stability, controlled drug release, terminability, and therapeutic effectiveness, our CAC ECT gel presents a promising therapeutic strategy for various retinal diseases in a clinical setting, eliminating the need for immunosuppressants.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142226766","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Chrysomycin A Reshapes Metabolism and Increases Oxidative Stress to Hinder Glioblastoma Progression 金霉素 A 重塑新陈代谢并增加氧化应激,从而阻碍胶质母细胞瘤的进展
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-29 DOI: 10.3390/md22090391
Dong-Ni Liu, Wen-Fang Zhang, Wan-Di Feng, Shuang Xu, Dan-Hong Feng, Fu-Hang Song, Hua-Wei Zhang, Lian-Hua Fang, Guan-Hua Du, Yue-Hua Wang
{"title":"Chrysomycin A Reshapes Metabolism and Increases Oxidative Stress to Hinder Glioblastoma Progression","authors":"Dong-Ni Liu, Wen-Fang Zhang, Wan-Di Feng, Shuang Xu, Dan-Hong Feng, Fu-Hang Song, Hua-Wei Zhang, Lian-Hua Fang, Guan-Hua Du, Yue-Hua Wang","doi":"10.3390/md22090391","DOIUrl":"https://doi.org/10.3390/md22090391","url":null,"abstract":"Glioblastoma represents the predominant and a highly aggressive primary neoplasm of the central nervous system that has an abnormal metabolism. Our previous study showed that chrysomycin A (Chr-A) curbed glioblastoma progression in vitro and in vivo. However, whether Chr-A could inhibit orthotopic glioblastoma and how it reshapes metabolism are still unclear. In this study, Chr-A markedly suppressed the development of intracranial U87 gliomas. The results from airflow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) indicated that Chr-A improved the abnormal metabolism of mice with glioblastoma. Key enzymes including glutaminase (GLS), glutamate dehydrogenases 1 (GDH1), hexokinase 2 (HK2) and glucose-6-phosphate dehydrogenase (G6PD) were regulated by Chr-A. Chr-A further altered the level of nicotinamide adenine dinucleotide phosphate (NADPH), thus causing oxidative stress with the downregulation of Nrf-2 to inhibit glioblastoma. Our study offers a novel perspective for comprehending the anti-glioma mechanism of Chr-A, highlighting its potential as a promising chemotherapeutic agent for glioblastoma.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211372","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Single Amino Acid Substitution in Loop1 Switches the Selectivity of α-Conotoxin RegIIA towards the α7 Nicotinic Acetylcholine Receptor 环路1中的单个氨基酸取代可改变α-芋螺毒素RegIIA对α7烟碱乙酰胆碱受体的选择性
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-29 DOI: 10.3390/md22090390
Jinpeng Yu, Junjie Xie, Yuting Ma, Pengcheng Wei, Panpan Zhang, Zepei Tang, Xiaopeng Zhu, Dongting Zhangsun, Sulan Luo
{"title":"Single Amino Acid Substitution in Loop1 Switches the Selectivity of α-Conotoxin RegIIA towards the α7 Nicotinic Acetylcholine Receptor","authors":"Jinpeng Yu, Junjie Xie, Yuting Ma, Pengcheng Wei, Panpan Zhang, Zepei Tang, Xiaopeng Zhu, Dongting Zhangsun, Sulan Luo","doi":"10.3390/md22090390","DOIUrl":"https://doi.org/10.3390/md22090390","url":null,"abstract":"α-Conotoxins are disulfide-rich peptides obtained from the venom of cone snails, which are considered potential molecular probes and drug leads for nAChR-related disorders. However, low specificity towards different nAChR subtypes restricts the further application of many α-conotoxins. In this work, a series of loop1 amino acid-substituted mutants of α-conotoxin RegIIA were synthesized, whose potency and selectivity were evaluated by an electrophysiological approach. The results showed that loop1 alanine scanning mutants [H5A]RegIIA and [P6A]RegIIA blocked rα7 nAChR with IC50s of 446 nM and 459 nM, respectively, while their inhibition against rα3β2 and rα3β4 subtypes was negligible, indicating the importance of the fifth and sixth amino acid residues for RegIIA’s potency and selectivity. Then, second-generation mutants were designed and synthesized, among which the analogues [H5V]RegIIA and [H5S]RegIIA showed significantly improved selectivity and comparable potency towards rα7 nAChR compared with the native RegIIA. Overall, these findings provide deep insights into the structure–activity relationship of RegIIA, as well as revealing a unique perspective for the further modification and optimization of α-conotoxins and other active peptides.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211371","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Comprehensive Assessment of Herbicide Toxicity on Navicula sp. Algae: Effects on Growth, Chlorophyll Content, Antioxidant System, and Lipid Metabolism 除草剂对 Navicula sp:对生长、叶绿素含量、抗氧化系统和脂质代谢的影响
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-28 DOI: 10.3390/md22090387
Chunyan Zheng, Jie Yang, Yunting Wang, Waqas Ahmed, Amir Khan, Jiannan Li, Jiechang Weng, Sajid Mehmood, Weidong Li
{"title":"Comprehensive Assessment of Herbicide Toxicity on Navicula sp. Algae: Effects on Growth, Chlorophyll Content, Antioxidant System, and Lipid Metabolism","authors":"Chunyan Zheng, Jie Yang, Yunting Wang, Waqas Ahmed, Amir Khan, Jiannan Li, Jiechang Weng, Sajid Mehmood, Weidong Li","doi":"10.3390/md22090387","DOIUrl":"https://doi.org/10.3390/md22090387","url":null,"abstract":"This study investigated the effects of herbicide exposure on Navicula sp. (MASCC-0035) algae, focusing on growth density, chlorophyll content, antioxidant system, and lipid metabolism. Navicula cultures were exposed to different concentrations of atrazine (ATZ), glyphosate (Gly), and acetochlor (ACT) for 96 h. Results showed a significant decrease in cell numbers, with higher herbicide concentrations having the most noticeable impacts. For instance, Gly-G2 had reduced cell populations by 21.00% at 96 h. Chlorophyll content varied, with Gly having a greater impact on chlorophyll a compared to ATZ and ACT. Herbicide exposure also affected the antioxidant system, altering levels of soluble sugar, soluble protein, and reactive oxygen species (ROS). Higher herbicide rates increased soluble sugar content (e.g., ATZ, Gly, and ACT-G2 had increased by 14.03%, 19.88%, and 19.83%, respectively, at 72 h) but decreased soluble protein content, notably in Gly-G2 by 11.40%, indicating cellular stress. Lipid metabolism analysis revealed complex responses, with changes in free proline, fatty acids, and lipase content, each herbicide exerting distinct effects. These findings highlight the multifaceted impacts of herbicide exposure on Navicula algae, emphasizing the need for further research to understand ecological implications and develop mitigation strategies for aquatic ecosystems.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211373","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Sulfated Aeruginosins from Lake Kinneret: Microcystis Bloom, Isolation, Structure Elucidation, and Biological Activity 来自基纳特湖的硫酸化麦角苷:微囊藻的繁殖、分离、结构解析和生物活性
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-28 DOI: 10.3390/md22090389
Shira Weisthal Algor, Assaf Sukenik, Shmuel Carmeli
{"title":"Sulfated Aeruginosins from Lake Kinneret: Microcystis Bloom, Isolation, Structure Elucidation, and Biological Activity","authors":"Shira Weisthal Algor, Assaf Sukenik, Shmuel Carmeli","doi":"10.3390/md22090389","DOIUrl":"https://doi.org/10.3390/md22090389","url":null,"abstract":"Aeruginosins are common metabolites of cyanobacteria. In the course of re-isolation of the known aeruginosins KT608A and KT608B for bioassay studies, we isolated three new sulfated aeruginosins, named aeruginosins KT688 (1), KT718 (2), and KT575 (3), from the extract of a Microcystis cell mass collected during the 2016 spring bloom event in Lake Kinneret, Israel. The structures of the new compounds were established on the basis of analyses of the 1D and 2D NMR, as well as HRESIMS data. Marfey’s method, coupled with HR ESI LCMS and chiral HPLC, was used to establish the absolute configuration of the amino acid and hydroxyphenyl lactic acid residues, respectively. Compounds 1–3 were tested for inhibition of the serine protease trypsin, and compounds 1 and 2 were found to exhibit IC50 values of 2.38 and 1.43 µM, respectively.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142226776","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Marine Bacteriocins: An Evolutionary Gold Mine to Payoff Antibiotic Resistance 海洋细菌素:消除抗生素耐药性的进化金矿
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-28 DOI: 10.3390/md22090388
Piyush Baindara, Roy Dinata, Santi M. Mandal
{"title":"Marine Bacteriocins: An Evolutionary Gold Mine to Payoff Antibiotic Resistance","authors":"Piyush Baindara, Roy Dinata, Santi M. Mandal","doi":"10.3390/md22090388","DOIUrl":"https://doi.org/10.3390/md22090388","url":null,"abstract":"The rapid evolution of drug resistance is one of the greatest health issues of the 21st century. There is an alarming situation to find new therapeutic strategies or candidate drugs to tackle ongoing multi-drug resistance development. The marine environment is one of the prime natural ecosystems on Earth, the majority of which is still unexplored, especially when it comes to the microbes. A wide variety of bioactive compounds have been obtained from a varied range of marine organisms; however, marine bacteria-produced bacteriocins are still undermined. Owing to the distinct environmental stresses that marine bacterial communities encounter, their bioactive compounds frequently undergo distinct adaptations that confer on them a variety of shapes and functions, setting them apart from their terrestrial counterparts. Bacterially produced ribosomally synthesized and posttranslationally modified peptides (RiPPs), known as bacteriocins, are one of the special interests to be considered as an alternative to conventional antibiotics because of their variety in structure and diverse potential biological activities. Additionally, the gut microbiome of marine creatures are a largely unexplored source of new bacteriocins with promising activities. There is a huge possibility of novel bacteriocins from marine bacterial communities that might come out as efficient candidates to fight against antibiotic resistance, especially in light of the growing pressure from antibiotic-resistant diseases and industrial desire for innovative treatments. The present review summarizes known and fully characterized marine bacteriocins, their evolutionary aspects, challenges, and the huge possibilities of unexplored novel bacteriocins from marine bacterial communities present in diverse marine ecosystems.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211374","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nutritional Value and Productivity Potential of the Marine Microalgae Nitzschia laevis, Phaeodactylum tricornutum and Isochrysis galbana 海洋微藻 Nitzschia laevis、Phaeodactylum tricornutum 和 Isochrysis galbana 的营养价值和生产潜力
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-27 DOI: 10.3390/md22090386
Xue Lu, Shufang Yang, Yongjin He, Weixuan Zhao, Man Nie, Han Sun
{"title":"Nutritional Value and Productivity Potential of the Marine Microalgae Nitzschia laevis, Phaeodactylum tricornutum and Isochrysis galbana","authors":"Xue Lu, Shufang Yang, Yongjin He, Weixuan Zhao, Man Nie, Han Sun","doi":"10.3390/md22090386","DOIUrl":"https://doi.org/10.3390/md22090386","url":null,"abstract":"Microalgae are considered promising sustainable feedstocks for the production of food, food additives, feeds, chemicals and various high-value products. Marine microalgae Phaeodactylum tricornutum, Isochrysis galbana and Nitzschia laevis are rich in fucoxanthin, which is effective for weight loss and metabolic diseases. The selection of microalgae species with outstanding nutritional profiles is fundamental for novel foods development, and the nutritional value of P. tricornutum, I. galbana and N. laevis are not yet fully understood. Hence, this study investigates and analyzes the nutritional components of the microalgae by chromatography and mass spectrometry, to explore their nutritional and industrial application potential. The results indicate that the three microalgae possess high nutritional value. Among them, P. tricornutum shows significantly higher levels of proteins (43.29%) and amino acids, while I. galbana has the highest content of carbohydrates (25.40%) and lipids (10.95%). Notwithstanding that P. tricornutum and I. galbana have higher fucoxanthin contents, N. laevis achieves the highest fucoxanthin productivity (6.21 mg/L/day) and polyunsaturated fatty acids (PUFAs) productivity (26.13 mg/L/day) because of the competitive cell density (2.89 g/L) and the advantageous specific growth rate (0.42/day). Thus, compared with P. tricornutum and I. galbana, N. laevis is a more promising candidate for co-production of fucoxanthin and PUFAs.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211375","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New Bioactive Polyketides from the Mangrove-Derived Fungus Penicillium sp. SCSIO 41411 源自红树林的真菌青霉 SCSIO 41411 的新型生物活性多酮化合物
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-26 DOI: 10.3390/md22090384
Yi Chen, Jian Cai, Ziwei Xia, Chunmei Chen, Yonghong Liu, Lalith Jayasinghe, Xueni Wang, Xuefeng Zhou
{"title":"New Bioactive Polyketides from the Mangrove-Derived Fungus Penicillium sp. SCSIO 41411","authors":"Yi Chen, Jian Cai, Ziwei Xia, Chunmei Chen, Yonghong Liu, Lalith Jayasinghe, Xueni Wang, Xuefeng Zhou","doi":"10.3390/md22090384","DOIUrl":"https://doi.org/10.3390/md22090384","url":null,"abstract":"Three new polyketides, including three ester derivatives (1, 3, and 5) and a new natural product, which was a benzoquinone derivative, embelin A (4), together with nine known ones (2 and 6–13), were isolated from the mangrove-derived fungus Penicillium sp. SCSIO 41411. Their structures were determined by detailed NMR and MS spectroscopic analyses. The X-ray single-crystal diffraction analysis of 4 was described for the first time. Compound 9 displayed obvious inhibition against PDE4 with an inhibitory ratio of 40.78% at 10 μM. Compound 12 showed DPPH radical scavenging activity, with an EC50 of 16.21 µg/mL, compared to the positive control (ascorbic acid, EC50, 11.22 µg/mL). Furthermore, compound 4 exhibited cytotoxicity against PC-3 and LNCaP with IC50 values of 18.69 and 31.62 µM, respectively.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Machine Learning-Driven Discovery and Evaluation of Antimicrobial Peptides from Crassostrea gigas Mucus Proteome 机器学习驱动的巨钳鱼粘液蛋白质组抗菌肽的发现与评估
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-08-26 DOI: 10.3390/md22090385
Jingchen Song, Kelin Liu, Xiaoyang Jin, Ke Huang, Shiwei Fu, Wenjie Yi, Yijie Cai, Ziniu Yu, Fan Mao, Yang Zhang
{"title":"Machine Learning-Driven Discovery and Evaluation of Antimicrobial Peptides from Crassostrea gigas Mucus Proteome","authors":"Jingchen Song, Kelin Liu, Xiaoyang Jin, Ke Huang, Shiwei Fu, Wenjie Yi, Yijie Cai, Ziniu Yu, Fan Mao, Yang Zhang","doi":"10.3390/md22090385","DOIUrl":"https://doi.org/10.3390/md22090385","url":null,"abstract":"Marine antimicrobial peptides (AMPs) represent a promising source for combating infections, especially against antibiotic-resistant pathogens and traditionally challenging infections. However, traditional drug discovery methods face challenges such as time-consuming processes and high costs. Therefore, leveraging machine learning techniques to expedite the discovery of marine AMPs holds significant promise. Our study applies machine learning to develop marine AMPs, focusing on Crassostrea gigas mucus rich in antimicrobial components. We conducted proteome sequencing of C. gigas mucous proteins, used the iAMPCN model for peptide activity prediction, and evaluated the antimicrobial, hemolytic, and cytotoxic capabilities of six peptides. Proteomic analysis identified 4490 proteins, yielding about 43,000 peptides (8–50 amino acids). Peptide ranking based on length, hydrophobicity, and charge assessed antimicrobial potential, predicting 23 biological activities. Six peptides, distinguished by their high relative scores and promising biological activities, were chosen for bactericidal assay. Peptides P1 to P4 showed antimicrobial activity against E. coli, with P2 and P4 being particularly effective. All peptides inhibited S. aureus growth. P2 and P4 also exhibited significant anti-V. parahaemolyticus effects, while P1 and P3 were non-cytotoxic to HEK293T cells at detectable concentrations. Minimal hemolytic activity was observed for all peptides even at high concentrations. This study highlights the potent antimicrobial properties of naturally occurring oyster mucus peptides, emphasizing their low cytotoxicity and lack of hemolytic effects. Machine learning accurately predicted biological activity, showcasing its potential in peptide drug discovery.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-08-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142211377","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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